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Erleada

apalutamide
Androgen Receptor Inhibitor Janssen FDA Approved 2018
Indications Dosing Forms Contraindications Warnings Adverse Reactions Pharmacology Clinical Studies Tumor Types
1. Indications and Usage

Non-metastatic castration-resistant prostate cancer (nmCRPC); Metastatic castration-sensitive prostate cancer (mCSPC).

2. Dosage and Administration

240 mg orally once daily (four 60 mg tablets)
Take with or without food. Swallow whole.
Continue LHRH analogue concurrently or have had bilateral orchiectomy

3. Dosage Forms and Strengths

Tablets: 60 mg

4. Contraindications

Pregnancy (can cause fetal harm).

5. Warnings and Precautions
  • Seizure: In 0.2%. Permanently D/C if seizure occurs. Avoid in patients with history of seizures or predisposing conditions.
  • Falls and Fractures: Falls in 16%, fractures in 12% (vs 7% placebo). Evaluate fall/fracture risk. Consider bone-protective agents.
  • Ischemic Cardiovascular Events: In 4% (vs 3% placebo). Monitor cardiovascular health.
  • Rash: In 26% (Grade 3-4 in 6%). Includes maculopapular, generalized, and urticarial. Most within first 120 days.
  • Hypothyroidism: In 8%. Monitor TSH periodically.
6. Adverse Reactions
Most Common Adverse Reactions

Fatigue (39%), hypertension (25%), rash (26%), diarrhea (20%), nausea (18%), weight decreased (16%), arthralgia (16%), falls (16%), hot flush (14%), decreased appetite (12%), fracture (12%), peripheral edema (11%)

Fatigue
39%
Rash
26%
Hypertension
25%
Diarrhea
20%
Nausea
18%
Weight Decreased
16%
Arthralgia
16%
Falls
16%
Hot Flush
14%
Decreased Appetite
12%

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

12. Clinical Pharmacology
Mechanism of Action

Apalutamide is a next-generation androgen receptor (AR) inhibitor that binds directly to the ligand-binding domain of the AR. It inhibits AR nuclear translocation, DNA binding, and AR-mediated transcription. In preclinical models, apalutamide has no agonist activity at the AR (unlike first-generation anti-androgens). It achieves higher brain-to-plasma ratios than enzalutamide, suggesting lower CNS-related adverse effects.

Pharmacokinetics

Tmax: 2 hours. Half-life: approximately 3 days (active metabolite N-desmethyl-apalutamide: ~4 days). Protein binding: 96% (parent), 95% (metabolite). Metabolized by CYP2C8 and CYP3A4. Steady-state by Week 4. Excreted in urine (65%) and feces (24%).

14. Clinical Studies

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

Pivotal Clinical Trials
Additional Resources
📋 All Apalutamide Trials on ClinicalTrials.gov ↗ 📚 PubMed: Apalutamide Clinical Trials ↗
Approved Tumor Types
Prostate Cancer